Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1082 Vismodegib (GDC-0449) <1 mg/mL 84 mg/mL <1 mg/mL
S1146 Cyclopamine <1 mg/mL <1 mg/mL 2 mg/mL
S2151 Sonidegib (Erismodegib, NVP-LDE225) <1 mg/mL 97 mg/mL 97 mg/mL
S2157 Taladegib (LY2940680) <1 mg/mL 5 mg/mL 2 mg/mL
S3042 Purmorphamine <1 mg/mL 4 mg/mL <1 mg/mL
S7160 Glasdegib (PF-04449913) <1 mg/mL 47 mg/mL <1 mg/mL
S8597 LYN-1604 100 mg/mL 50 mg/mL 100 mg/mL
S2777 PF-5274857 93 mg/mL 93 mg/mL <1 mg/mL
S8075 GANT61 <1 mg/mL <1 mg/mL 12 mg/mL
S7092 SANT-1 <1 mg/mL 21 mg/mL 20 mg/mL
S7138 BMS-833923 <1 mg/mL 95 mg/mL <1 mg/mL
S8200 MK-4101 <1 mg/mL 98 mg/mL 60 mg/mL
S8249 HPI-4 (Ciliobrevin A) <1 mg/mL 71 mg/mL 1 mg/mL
S4747 Jervine <1 mg/mL 5 mg/mL 2 mg/mL
S7779 Smoothened Agonist (SAG) HCl 100 mg/mL 71 mg/mL 40 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations

Vismodegib (GDC-0449)

Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay.



Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.


Sonidegib (Erismodegib, NVP-LDE225)

Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.


Taladegib (LY2940680)

Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.



Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM.


Glasdegib (PF-04449913)

Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.



LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.



PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.



GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.



SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.



BMS-833923 is an orally bioavailable Smoothened antagonist. Phase 2.



MK-4101, a potent inhibitor of the Hedgehog pathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells.


HPI-4 (Ciliobrevin A)

HPI-4 (Ciliobrevin A) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo.



Jervine is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened.


Smoothened Agonist (SAG) HCl

Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.

Tags: Smo activity | smoothened pathway | smoothened pathway | smoothened signaling | Smo cancer | Smo pathway | smoothened signaling pathway | smoothened inhibitor review